An amount of 5 g (11.3 mmol) of betulin (1) and DMAP (3.05 g, 25 mmol) were placed in a round-bottomed flask, in 200 mL of dry pyridine, at 0 °C (cooling bath). Then, 24.5 mL (0.25 mmol) of Ac2O was slowly added dropwise (over 1 h) to the stirred solution from the additional funnel. The solvent was evaporated under reduced pressure to give a crude dark solid, which was purified by column chromatography in the system hexane:ethyl acetate (H:OAc) 40:1→5:1 v/v, to deliver first 0.55 g (11%) of betulin 3,28-diacetate 3 as a w white crystalline powder, then 1.86 g (37%) of betulin 28-acetate as a white crystalline powder.

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